Thursday, October 18, 2012
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Small cell lung cancer
B cell lymphoma 2
Cell culture and mouse
studies identified inhibitors of BCL-2 and Bcl-XL that could help
treat small cell lung cancer. In human small cell lung cancer lines, 4,5-diphenyl-1H-pyrrole-3-carboxylic
acid-based BCL-2 and Bcl-XL inhibitors designed
using structure-based optimization induced cell death more potently than
clinical-stage inhibitors, including ABT-263.
In mouse xenograft models of human small cell lung cancer, the most potent
inhibitor induced apoptosis and tumor regression that prevented tumor growth
for at least 15 days. Next steps could include testing the inhibitors in
additional animal models of small cell lung cancer.
Laboratories and Roche's
Inc. unit have the BCL-2-family protein inhibitor ABT-263
in Phase I/II testing to treat small cell lung cancer.
At least seven other companies have inhibitors of BCL-2-family proteins in
clinical and preclinical testing to treat cancers.
Published online Oct. 18, 2012
Patent and licensing status
Chen, J. et al. J. Med.
Chem.; published online Oct. 2, 2012;
Contact: Shaomeng Wang, University of Michigan, Ann Arbor,
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